Drug reference

glecaprevir

NS3 protease inhibitor · Antiviral, Hepatitis C agent

NS3 protease inhibitorAntiviral, Hepatitis C agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

Hiv Protease InhibitorsSevereTextbookG&G 14e · p1241
Potent Cyp3a InducersSevereTextbookG&G 14e · p1241, p1242
Potent Oatp1b1 InhibitorsSevereTextbookG&G 14e · p1241, p1242
Potent P Gp InducersSevereTextbookG&G 14e · p1241, p1242

Mechanism

Glecaprevir is an inhibitor of the non-structural protein 3 (NS3) protease of the hepatitis C virus, which is essential for viral polyprotein processing and replication.

Indications

All HCV genotypes (pangenotypic) for treatment-naïve individuals (as part of fixed-dose combination with pibrentasvir)Treatment-experienced patients with prior NS3 protease and NS5A failures (as part of fixed-dose combination with pibrentasvir)HCV in patients with chronic kidney disease (preferred treatment in renal impairment)Children aged >12 years or ≥45 kg (as part of fixed-dose combination with pibrentasvir)Children aged ≥3 years (weight-based dosing of film-coated pellets, as part of fixed-dose combination with pibrentasvir)

Dosing

Adult: 300 mg (as part of three fixed-dose combination tablets with pibrentasvir) once daily for 8 weeks
Pediatric: 250 mg (as part of GLE/PIB) for children weighing ≥30 kg to <45 kg; 200 mg for children weighing ≥20 kg to <30 kg; 150 mg for children weighing 12 kg to <20 kg
Renal adjustment: Preferred treatment in renal impairment, though exposures are elevated in ESRD

Pharmacokinetics

Half-life

6 h

Protein binding

Highly protein-bound

Metabolism

Substrate of CYP3A and OATP1B1/3

Excretion

Largely via biliary-fecal route (>92%); renal excretion less than 1%

Contraindications

Decompensated cirrhosis
Advanced liver disease
Concomitant use with potent P-gp, CYP3A inducers (antiepileptics, St. John’s wort, rifampin, efavirenz)
Concomitant use with HIV protease inhibitors or cyclosporine (due to increased GLE exposures and potential hepatotoxicity)
Concomitant use with ethinyl estradiol-containing hormonal contraception (during and for 2 weeks after treatment)